2种盐酸非索非那定制剂的人体生物等效性研究

Study on Bioequivalence of 2 Kinds of Fexofenadine Hydrochloride Agents in Human

目的:研究盐酸非索非那定口腔崩解片与普通片在正常人体内的生物等效性。方法:采用随机双周期交叉试验设计,20名男性健康志愿者分别单剂量口服盐酸非索非那定口腔崩解片(受试制剂)与普通片(参比制剂)60mg,采用高效液相色谱-电喷雾串联质谱(LC-MS/MS)法测定非索非那定血药浓度,用DASver2.1软件计算二者药动学参数以考察生物等效性。结果:受试者单剂量口服受试制剂与参比制剂后的Cmax分别为(240.01±77.66)、(237.76±89.97)ng·mL-1,tmax分别为(1.85±1.02)、(2.18±0.81)h,AUC0～72分别为(1309.9±467.7)、(1236.3±433.1)ng·h·mL-1,AUC0～∞分别为(1319.2±468.8)、(1245.9±436.2)ng·h·mL-1。受试制剂相对于参比制剂的生物利用度为(112±36)%。结论:盐酸非索非那定口腔崩解片与普通片具有生物等效性。

OBJECTIVE： To study bioequivalence of fexofenadine hydrochloride orally disintegrating tablets and fexofenadine hydrochloride conventional tablets. METHODS： In two-period cross-over design test, 20 healthy male volunteers were given a single oral dose of 60 mg fexofenadine hydrochloride orally disintegrating tablet （test tablet） and 60 mg fexofenadine hydrochloride conventional tablet （reference tablet）. Plasma concentration of fexofenadine was determined by LC-MS/MS. Bioavailability and pharmacokinetic parameters were evaluated by DAS ver 2.1 software. RESULTS： Main pharmacokinetic parameters of test vs. reference tablets were as follows： Cmax（240.01 ± 77.66） ng.mL^-1 vs. （237.76 ± 89.97） ng·mL^-1; tmax（1.85 ± 1.02） h vs. （2.18 ± 0.81）h; AUC0-72（1 309.9 ± 467.7） ng·h·mL^-1 vs. （1 236.3 ± 433.1） ng·h·mL^-1; AUC0-∞（1 319.2 ± 468.8） ng·h·mL^-1 vs. （1 245.9 ± 436.2） ng·h·mL^-1. As compared with reference tablet, the bioavailability of the test tablet was （112 ± 36） %. CONCLUSION： The statistic result shows the test and reference tablets are bioequivalent.